📜2-(2-溴乙基)吡啶氢溴酸盐置于sodium Hydroxide体系中,用95%的收率获得2-(2-溴乙基)吡啶 参考文献:Spiro Derivatives Of Tetrahydrothiophene. Synthesis Of The Quinolizidine <3-Spiro-2'> Tetrahydrothiophene System Using Solid/liquid Or Liquid/liquid Phase-Transfer Catalysis 标题:Spiro Derivatives Of Tetrahydrothiophene. Synthesis Of The Quinolizidine <3-Spiro-2'> Tetrahydrothiophene System Using Solid/liquid Or Liquid/liquid Phase-Transfer Catalysis 摘要:4-氧代八氢喹啉<3-螺-2'>四氢噻吩1',1'-二氧化物可以通过两条独立的途径从2-氰基四氢噻吩合成,两者均使用相转移催化:第一条途径涉及在ptc条件下对2-氰基四氢噻吩进行烷基化,第二条途径则是使用2-氯乙基哌啶与2-氯羰基四氢噻吩进行n-酰化,最后在ptc条件下进行环烷基化.得到两个螺旋化合物的立体异构体. Doi:10.1055/s-1987-33430
专利号:US-7692019-B2 优先权日:2000-12-04 标 题:Methods for the stereoselective synthesis of substituted piperidines 发明人:AQUILA BRIAN M; BANNISTER THOMAS D; CUNY GREGORY D; HAUSKE JAMES R; HEFFERNAN MICHELE L R; HOEMANN MICHAEL Z; KESSLER DONALD W; SHAO LIMING; WU XINHE; XIE ROGER L 权利人:SEPRACOR INC 摘要:One aspect of the present invention relates to methods of synthesizing substituted piperidines. A second aspect of the present invention relates to stereoselective methods of synthesizing substituted piperidines. The methods of the present invention will find use in the synthesis of compounds useful for treatment of numerous ailments, conditions and diseases that afflict mammals, including but not limited to addiction and pain. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the substituted piperidines using the methods of the present invention. An additional aspect of the present invention relates to enantiomerically substituted pyrrolidines, piperidines, and azepines.
专利号:US-2025129021-A1 优先权日:2023-09-19 标 题:Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I), Formula (V)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
专利号:US-4486572-A 优先权日:1983-07-06 标 题 :Synthesis of amphiphilic block copolymers and networks 发明人:KENNEDY JOSEPH P 权利人:UNIV AKRON 摘要:A novel terminally functional (i.e., telechelic) polymers having a polyisobutylene are described. The end groups are styryl and can be reacted with conventional monomers to form copolymers having unique physical properties. Copolymerizations with N-vinyl-2-pyrrolidone produce amphiphilic polymers which are useful in the areas of medicine and agricultural chemicals.
专利号:US-6872716-B2 优先权日:2000-09-11 标题:Antipsychotic sulfonamide-heterocycles, and methods of use thereof 发明人:WU XINHE; AQUILA BRIAN M; SHAO LIMING; RADEKE HEIKE; CUNY GREGORY D; HAUSKE JAMES R; XIE ROGER L 权利人:SEPRACOR INC 摘要:One aspect of the present invention relates to heterocyclic compounds comprising a sulfonamide moiety. A second aspect of the present invention relates to the use of the heterocyclic compounds comprising a sulfonamide moiety to treat diseases, afflictions or maladies caused at least in part by abnormal activity of one or more GPCRs or ligand-gated ion channels. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds comprising a sulfonamide moiety, and the screening of those libraries for biological activity, e.g., in animal models of psychosis.
专利号:WO-2004058727-A1 优先权日:2002-12-20 标题 :Substituted 3,5-dihydro-4h-imidazol-4-ones for the treatment of obesity 发明人:CHEN YUANWEI; O'CONNOR STEPHEN JAMES; GUNN DAVID; NEWCOM JASON; CHEN JIANQING; YI LIN; ZHANG HAI-JUN; HUNYADI LASZLO MATYAS; NATERO REINA 权利人:BAYER PHARMACEUTICALS CORP; CHEN YUANWEI; O'CONNOR STEPHEN JAMES; GUNN DAVID; NEWCOM JASON; CHEN JIANQING; YI LIN; ZHANG HAI-JUN; HUNYADI LASZLO MATYAS; NATERO REINA 摘要:This invention relates to substituted 3,5-dihydro-4H-imidazol-4-ones compounds which are useful in the treatment of obesity and obesity-related disorders, and as weight-loss and weight-control agents. The invention also provides methods for synthesis of the compounds, pharmaceutical compositions comprising the compounds, and methods of using such compositions for inducing weight loss and treating obesity and obesity-related disorders.
专利号:US-2002177721-A1 优先权日:2000-12-04 标题 :Methods for the stereoselective synthesis of substituted piperidines